metastases

Sivifene is a antitumor agent. Sivifene can be used for research on the treatment of cutaneous metastases from cancer.

N-[2-(diethylamino)ethyl]-2-iodobenzamide is a radiopharmaceutical for the scintigraphic detection of melanoma and metastases.

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

Ned 19, a selective membrane-permeant non-competitive antagonist of NAADP, strongly inhibits tumor growth, vascularization, and lung metastases in mice.

Efaproxiral Sodium (RSR13 sodium), a synthetic allosteric modifier of hemoglobin, is utilized for brain metastases originating from breast cancer.

CS1 peptide is present within type III homology connecting segment (IIICS) as well as C-274 (cell-binding domain). Fibronectin CS1 Peptide lacks the Arg-Gly-Asp-containing domain, actively inhibits tumor metastases in spontaneous and experimental metastas

ATN-161 trifluoroacetate salt (ATN-161 TFA salt) is a novel integrin α5β1 antagonist that inhibits angiogenesis and growth of liver metastases and improves survival in a murine model.

ATN-161, a novel integrin α5β1 antagonist, inhibits angiogenesis and the growth of liver metastases in a murine model.

TAS2940 is an irreversible pan-ERBB inhibitor with enhanced brain penetration, utilized for treating lung cancer brain metastases and glioblastomas with HER2 EGFR exon 20 insertions and EGFR abnormalities. In intracranial xenograft models of HER2 EGFR cancers, TAS2940 has demonstrated efficacy in improving survival rates in mice. Currently, TAS2940 is undergoing Phase I clinical trials to establish the maximum tolerated dose for solid tumors.

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

PF-5274857 hydrochloride is a potent, orally active, selective Smo antagonist (IC50=5.8 nM, Ki=4.6 nM) that is permeable through the blood-brain barrier. It has research potential in various tumors, including brain tumors and brain metastases driven by activated Hh pathways.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

C17 Lactosylceramide is a naturally occurring sphingolipid that has been found in human brain metastases of lung adenocarcinomas but not in healthy brain tissue.

DOTA Zoledronate represents a novel, advanced compound utilized specifically in bone-targeted radionuclide therapy to diagnose bone metastases.

Kadsurenone is a platelet-activating factor receptor antagonist from Chinese herbal plant, haifenteng. It is a useful and promising treatment strategy for breast cancer bone metastases by blocking the PAF PTAFR signaling pathway.

Etanidazole (SR-2508) is a 2-nitroimidazole drug with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

VEL-0230, also known as NC-2300, is a potent cathespin K inhibitor. VEL-0230 has dual-acting properties that both stimulates bone formation and inhibits loss. VEL-0230 is being studied preclinically for the treatment of diseases involving bone mineral disorders such as bone loss related to multiple myeloma, osteoporosis, bone metastases, and rheumatoid arthritis. Velcura Therapeutics is currently being developed by Velcura Therapeutics. Given VEL- 0230's promotion of bone formation, inhibition of bone loss and reduction of calcium levels, Velcura has chosen Myeloma as its lead indication, as the bone fragility, bone pain, high calcium levels and eventual kidney involvement present serious medical and quality of life issues to affected patients.

Nemorubicin HCL is the salt form of Nemorubicin, also known as PNU152243A, a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

KRAS G12D inhibitor 15 is a potent and specific inhibitor targeting the KRAS G12D mutation, showing potential for research into various diseases and disorders, including cancer and its metastases [1].

Isoxanthohumol is a prenylated flavonoid derived from hops and beer with antiproliferative activity against several human cancer cell lines.Isoxanthohumol inhibits the metastasis or invasion of lung metastases of tumor cells.Isoxanthohumol has antiviral activity against herpesviruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV).

Intetumumab (CNTO 95) is a fully human anti-α(v)-integrin monoclonal antibody that is a radiosensitizer in xenograft tumor-bearing mice, inhibits tumor growth, and reduces lung metastases in the A549 NSCLC xenograft model.

DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist with the molecular structure p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2, used for in vivo tumor tracing via isotopic labeling, such as 177Lu-DOTA-LM3 TFA and 68Ga-DOTA-LM3 TFA. The 68Ga-labeled compound shows favorable biodistribution, high tumor uptake, good tumor retention, and minimal safety concerns, while the 177Lu-labeled variant targets DOTATOC-negative liver metastases, including pancreatic NET and extensive tumor thrombosis [1] [2].